WEEK 1
CH 81
Pharmacokinetics of Amphotericin B
Drug class: Polyene antifungal agent. They are ineffective against many systemic fungal
infections and are only available IV.
MOA: binds to components of the fungal membrane increasing permeability. Resulting in
intracellular leakage, reducing organism viability. Depending on the agents concentration and
fungal susceptibility, the action could be fungistatic or fungicidal.
Unique feature: Amphotericin B binds to the ergosterol component (Member of the sterol
family) of the fungal membrane. For a cell to be susceptible, its membrane must contain
sterols. Bacterial membranes lack sterols; this agent is ineffective against bacteria. Drug of
choice for most systemic mycoses.
Amphotericin B: Minimizing Nephrotoxicity
Adverse effect is nephrotoxicity. The risk is dose dependent. If the total dose exceeds 4g, renal
impairment is likely. Dosage should be reduced in patients with renal impairments. The drug
should also be administered for the shortest time possible. Treatment is usually 6-8 weeks but
may last 3-4 months. Avoid combining this medication with other nephrotoxic agents including
aminoglycosides, cyclosporins, NSAID’s
Itraconazole Drug Interactions
PPI- Since PPI have a prolonged duration of action, patient using these agents may have
insufficient stomach acid content for itraconazole absorption.
Cisapride, pimozide, dofetilide, and quinidine- Itraconazole is a CYP2A4 inhibitor and can
increase levels of many other drugs, including Cisapride, pimozide, dofetilide, and quinidine
which can increase the risk of fatal ventricular dysrhythmias.
Antacids, PPI, H2 Receptor antagonist- drugs that raise gastric pH can reduce the
absorption of oral itraconazole. Administer these agents at least 1 hour before itraconazole or
2 hours after.
Azole Use in Older Adults
The risk of achlorhydria (absent or reduced gastric hydrochloric production) is greater in older
adults. This condition could make absorption of some antifungal agents unpredictable. Plasma
levels of commonly prescribed medications in older adults (warfarin, phenytoin, oral
hypoglycemics) are increased in azoles. Med rec and safety with poly-pharmacy practice
should be prioritized.
Therapeutic Uses of Caspofungin
Systemic fungal infection, approved for IV therapy for invasive aspergillosis in clients
unresponsive or intolerant to amphotericin b or itraconazole or systemic candida infections,
including candidemia and candida-related peritonitis, pleural space infections, and
intraabdominal abscesses. Drug class: Echinocandin antifungal agent. Primary function:
narrow-spectrum IV antifungal agent limited to aspergillus and candida species. Unique
feature: These drugs are the newest class of antifungal agents. In contrast to amphotericin B
and the azoles, which disrupt the fungal cell membrane, the echinocandins disrupt the fungal
cell wall. Caspofungin is better tolerated than amphotericin b with similar efficiency.
Adverse Effects of Caspofungin
Rash, facial flush, pruritic, anaphylaxis, or a sense of warmth related to histamine response
(histamine-mediated reactions), phlebitis at injection site, common reactions include fever,
headache, rash, nausea, vomiting. Avoid use in pregnancy unless benefit outweigh the risk.
, Reduce dosage in patient with moderate hepatic impairment. Contraindicated in patient with
severe hepatic impairment.
Griseofulvin Indications
The first oral antifungal treatment of infection caused by dermatophytes. It is approved to treat
superficial dermatophyic infections of the skin and nails that do not respond to topical therapy.
Specifically, it is employed to treat tinea barbae, tinea capitis, tinea corporis, and tinea cruris. It
is also used to treat onychomycosis. It is effective against fungal infections caused by
trichophyton spp., Epidermophyton floccosum, microsporum audouini, microsporum Canis,
and microsporum gypseum. The drug is not active against candida species, nor is it useful
against systemic mycoses.
Oral Terbinafine Indications
Used for treatment of onychomycosis, a fungal infection of the toenails and fingernails caused
by tinea unguium the infection often causes nail thickening and deformity. Off label use to treat
tinea infections and sporotrichosis (rose gardener’s disease), a fungal disease spread through
spores in soil and plant matter.
Tinea Pedis Treatment
Defined by location: Tinea pedis (ringworm of the foot), the most common fungal infection
generally responds well to topical therapy, azole or allylamine. Treatment should continue for
at least 1 week after symptoms have cleared. Severe infection may require systemic antifungal
agent. Advise patients to wear absorbent cotton socks, change shoes often, and dry their feet
after bathing.
Treatment Choice for Systemic Mycoses
Treating systemic mycoses can be difficult: these infections often resist treatment and hence
may require prolonged therapy with drugs that frequently prove toxic. All formulations are given
IV infusion either daily or every other day for several months. Amphotericin B is a drug of
choice for most systemic mycoses. This drug is highly toxic with infusion reaction and renal
damage. Reserved for infections that are progressive and potentially fatal.
CH 82
Acyclovir MOA
Acyclovir inhibits viral DNA synthesis by undergoing activation to acyclo-guanosine
monophosphate (GMP) via the thymidine kinase enzyme. GMP is then converted to acyclo-
guanosine triphosphate (GTP) which then inhibits viral DNA polymerase and gets incorporated
into viral DNA, blocking further DNA chain growth. Acyclovir specifically targets viral DNA
synthesis, minimizing effects on human cells.
Acyclovir Indication
Herpes simplex virus (HSV), varicella zoster virus (VZV), and cytomegalovirus (CMV).
Acyclovir: Route of Administration Considerations
Topical, oral, or IV. Administration of IV is over one hour. When applying topical use, a finger
cot or glove to prevent spreading the virus to other areas or people. The medication does not
cure HSV. Practice good hand hygiene to reduce risk of spreading. Avoid sexual contact
during genital outbreaks.
Oseltamivir (Tamiflu) MOA
MOA: Inhibits the neuraminindase enzyme on the surface of the influenza virus. This inhibition
prevents the release of new viral particles from infected cells, effectively halting the spread of
infection within the body. Unique feature: also effective against certain pandemic strains like
H1N1 (swine flu) and H5N1 (avian flu)
Oseltamivir (Tamiflu) Administration
CH 81
Pharmacokinetics of Amphotericin B
Drug class: Polyene antifungal agent. They are ineffective against many systemic fungal
infections and are only available IV.
MOA: binds to components of the fungal membrane increasing permeability. Resulting in
intracellular leakage, reducing organism viability. Depending on the agents concentration and
fungal susceptibility, the action could be fungistatic or fungicidal.
Unique feature: Amphotericin B binds to the ergosterol component (Member of the sterol
family) of the fungal membrane. For a cell to be susceptible, its membrane must contain
sterols. Bacterial membranes lack sterols; this agent is ineffective against bacteria. Drug of
choice for most systemic mycoses.
Amphotericin B: Minimizing Nephrotoxicity
Adverse effect is nephrotoxicity. The risk is dose dependent. If the total dose exceeds 4g, renal
impairment is likely. Dosage should be reduced in patients with renal impairments. The drug
should also be administered for the shortest time possible. Treatment is usually 6-8 weeks but
may last 3-4 months. Avoid combining this medication with other nephrotoxic agents including
aminoglycosides, cyclosporins, NSAID’s
Itraconazole Drug Interactions
PPI- Since PPI have a prolonged duration of action, patient using these agents may have
insufficient stomach acid content for itraconazole absorption.
Cisapride, pimozide, dofetilide, and quinidine- Itraconazole is a CYP2A4 inhibitor and can
increase levels of many other drugs, including Cisapride, pimozide, dofetilide, and quinidine
which can increase the risk of fatal ventricular dysrhythmias.
Antacids, PPI, H2 Receptor antagonist- drugs that raise gastric pH can reduce the
absorption of oral itraconazole. Administer these agents at least 1 hour before itraconazole or
2 hours after.
Azole Use in Older Adults
The risk of achlorhydria (absent or reduced gastric hydrochloric production) is greater in older
adults. This condition could make absorption of some antifungal agents unpredictable. Plasma
levels of commonly prescribed medications in older adults (warfarin, phenytoin, oral
hypoglycemics) are increased in azoles. Med rec and safety with poly-pharmacy practice
should be prioritized.
Therapeutic Uses of Caspofungin
Systemic fungal infection, approved for IV therapy for invasive aspergillosis in clients
unresponsive or intolerant to amphotericin b or itraconazole or systemic candida infections,
including candidemia and candida-related peritonitis, pleural space infections, and
intraabdominal abscesses. Drug class: Echinocandin antifungal agent. Primary function:
narrow-spectrum IV antifungal agent limited to aspergillus and candida species. Unique
feature: These drugs are the newest class of antifungal agents. In contrast to amphotericin B
and the azoles, which disrupt the fungal cell membrane, the echinocandins disrupt the fungal
cell wall. Caspofungin is better tolerated than amphotericin b with similar efficiency.
Adverse Effects of Caspofungin
Rash, facial flush, pruritic, anaphylaxis, or a sense of warmth related to histamine response
(histamine-mediated reactions), phlebitis at injection site, common reactions include fever,
headache, rash, nausea, vomiting. Avoid use in pregnancy unless benefit outweigh the risk.
, Reduce dosage in patient with moderate hepatic impairment. Contraindicated in patient with
severe hepatic impairment.
Griseofulvin Indications
The first oral antifungal treatment of infection caused by dermatophytes. It is approved to treat
superficial dermatophyic infections of the skin and nails that do not respond to topical therapy.
Specifically, it is employed to treat tinea barbae, tinea capitis, tinea corporis, and tinea cruris. It
is also used to treat onychomycosis. It is effective against fungal infections caused by
trichophyton spp., Epidermophyton floccosum, microsporum audouini, microsporum Canis,
and microsporum gypseum. The drug is not active against candida species, nor is it useful
against systemic mycoses.
Oral Terbinafine Indications
Used for treatment of onychomycosis, a fungal infection of the toenails and fingernails caused
by tinea unguium the infection often causes nail thickening and deformity. Off label use to treat
tinea infections and sporotrichosis (rose gardener’s disease), a fungal disease spread through
spores in soil and plant matter.
Tinea Pedis Treatment
Defined by location: Tinea pedis (ringworm of the foot), the most common fungal infection
generally responds well to topical therapy, azole or allylamine. Treatment should continue for
at least 1 week after symptoms have cleared. Severe infection may require systemic antifungal
agent. Advise patients to wear absorbent cotton socks, change shoes often, and dry their feet
after bathing.
Treatment Choice for Systemic Mycoses
Treating systemic mycoses can be difficult: these infections often resist treatment and hence
may require prolonged therapy with drugs that frequently prove toxic. All formulations are given
IV infusion either daily or every other day for several months. Amphotericin B is a drug of
choice for most systemic mycoses. This drug is highly toxic with infusion reaction and renal
damage. Reserved for infections that are progressive and potentially fatal.
CH 82
Acyclovir MOA
Acyclovir inhibits viral DNA synthesis by undergoing activation to acyclo-guanosine
monophosphate (GMP) via the thymidine kinase enzyme. GMP is then converted to acyclo-
guanosine triphosphate (GTP) which then inhibits viral DNA polymerase and gets incorporated
into viral DNA, blocking further DNA chain growth. Acyclovir specifically targets viral DNA
synthesis, minimizing effects on human cells.
Acyclovir Indication
Herpes simplex virus (HSV), varicella zoster virus (VZV), and cytomegalovirus (CMV).
Acyclovir: Route of Administration Considerations
Topical, oral, or IV. Administration of IV is over one hour. When applying topical use, a finger
cot or glove to prevent spreading the virus to other areas or people. The medication does not
cure HSV. Practice good hand hygiene to reduce risk of spreading. Avoid sexual contact
during genital outbreaks.
Oseltamivir (Tamiflu) MOA
MOA: Inhibits the neuraminindase enzyme on the surface of the influenza virus. This inhibition
prevents the release of new viral particles from infected cells, effectively halting the spread of
infection within the body. Unique feature: also effective against certain pandemic strains like
H1N1 (swine flu) and H5N1 (avian flu)
Oseltamivir (Tamiflu) Administration
